Hypothalamic and Pituitary Hormones

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  1. rhIGF-1/rhIGFBP-3 complex
    You are in MECca listening to a SERMon about food when you start to get hangery and EDGY from increased insulin and turn into a TYRant after 20 min. You are in the Mecca because GH didn't work! You know you are a child with growth failure and need to eat before you get hypoglycemic.

    • IGF1 analog --> insulin and EGF Try Kinase receptor
    • Children with growth failure
    • SC, 20min before or after meal
    • Hypoglycemia

  2. GH & GHRH Agonists MOA
    • Jak bought bean stalk beans to increase his insulin since he is
    • starving. The bean stalk grew leading to the Giant Tyrant's house! The Giant Tyrant says SERMORELIN! and Jak's soma trembles and tropins.

    GH agonist: JAK/STAT Try Kinase activator --> increase IGF1 (insulin-like growth factor)

    • Three drugs:
    • Sermorelin- GHRH homologue
    • Somatrem- rhGH
    • Somatropin- rhGH
  3. GH & GHRH Agonists Uses
    Jak also has to feed his siblings, Willie, Turner and AIDS, who are all short idiots with bowl cuts.

    • Uses:
    • Prader-Willie syndrome
    • Turner's syndrome
    • Wasting in AIDS
    • Short Bowel syndrome
    • Idiopathic short stature
  4. GH & GHRH Agonists SE
    • Children go to school and must:
    • Fill their craniums
    • Listen with their ears
    • Get scoliosis checks
    • Make energy with thyroid gland for E

    • Cranial: nausea/vomiting, visual changes, HA
    • Otitis media
    • Scoliosis
    • Hypothyroidism

    Adults: old people complain about joint pain (arthralgia), edema, myalgia and carpal tunnel because they are office slaves
  5. Growth Hormone Antagonist
    • Octreotide- Somatostatin (GHRIH) homologue
    • Pegvisomant- a GH receptor antagonist
  6. Tell me about Pegvisomant
    • GH-R anatagonist
    • Peg has acromegaly and wears a visor to make herself feel normal because she looks like a man.

    Acromegaly people take Pegvisomant to normalize their IGF1 levels.
  7. Tell me about Octreotide
    • Octopus says, "Don't go there" to the tumor
    • Somatostatin analog

    • Octopus keeps you from growing, being happy, acidifiying food, increasing blood sugar, having diarrhea and distending your stomach.
    • Use: sx from hormone secreting tumors
    • Acromegaly (GH)
    • Carcinoid tumor (serotonin)
    • Gastrinoma (gastrin)
    • Glucagonoma
    • Diabetes diarrhea
    • WDHA (vasoactive intestinal peptide)

    SE: Octopus has ink that makes you N/V, abd cramps, fart, gallstones, steatorrhea and B12 deficiency (malabsorption). He is soothing and decreases BPM (brady).
  8. FSH/LH preparation
    Menostropins (hMG)
  9. FSH preparations
    • Urofolitropin (uFSH)
    • Follitropin alpha, Follitropin beta (rFSH)
  10. LH preparation
    Lutropin (rLH)
  11. hCG preparation
    Choriogonadotropin alpha (rhCG)
  12. GnRH Agonists
    • Gonadorelin
    • Goserelin
    • Histrelin
    • Leuprolide
    • Nafarelin
    • Triptorelin
  13. GnRH Receptor Antagonists
    • Ganirelix
    • Cetrorelix
  14. Activin
    • Increase FSH
    • "Active people enjoy FreSH air!"
  15. Inhibin
    • Decrease FSH
    • "Inhibited people get less FreSH air"
  16. Estrogens
    • Decreases: MOA (increase serotonin), LDL, bone resorption
    • Increases: HDL, coagulation
    • breast enlargement (sexual maturity), endometrial lining, Liver metabolized.
    • MOA: Increases sex hormone binding globulin SHBG
    • Use: Hormone replacement therapy, Primary hypogonadism, suppress ovulation (IVT or birth control)
  17. Estrogen SE's and Contraindications
    • SE: bleeding, increase risk of cancer, adenocarcinoma in pregnant women, migraine, HTN, edema, cholestasis
    • Contraindications: undiagnosed vaginal bleeding, estrogen dependent cancer pt's, thromboembolic disorders, heavy smokers, liver disease pts
  18. Estrogen Analogs
    • Ethynyl Estradiol
    • Micronized Estradiol
    • Estradiol cypinoate
    • Estradiol valerate
    • Estropivate
    • Conjugated: Quinestrole (decreased hepatic effects), Chlorotrianisene, Methallenestril (both increase heptatic effects)
  19. Contraceptives
    • COC (estrogen and progesterone)
    • POC (progesterone only)
    • Use: antibabies, endometriosis, PMS, depression
    • MOA: Inhibits GnRH, FSH, LH (so no ovulation, no lining grows, no implantation)
  20. Contraceptive Adverse Effects
    • Mild: Migraine, edema, change in serum proteins
    • Moderate: acne, hirsutism, weight gain, break through bleeding, skin pigmentation
    • Severe: depression, MI, DVT, pulmonary embolism, increased risk stroke, vascular disease, GI disorders (especially gallbladders), cancer
  21. Contraceptive Drug Interactions
    • Drugs that increase liver metabolism will decrease this drugs effectiveness...
    • Antimicrobials: tetracycline, ampicillin, griseofulvin
    • Rifampin, and other P450 inducers
  22. Progesterone only contraceptives
    • medroxyprogesterone, DMPA
    • Used when pts can't use estrogen: liver disease, HTN, psychosis, prior thromboembolism.
    • NOT for people planning a pregnancy soon
    • SQ implantation
    • prolonged ovulation suppression
  23. Progesterone Side effects
    Dizziness, bloating, weight gain, reversible glucose intolterance, HA
  24. Post Coital Contraception
    • Mifepristone
    • Progesterone antagonist
    • MOA: luteolysis (degradation of corpus luteum)
    • Abortifactant: when combined w/ prostaglandin in E1 or misoprostol
  25. Side Effects of Mifepristone
    prolonged bleeding
  26. Progesterone - pregnancy hormone!
    • Metabolite in urine - pregnanediol glucoronide (pregnant & wants sugar)
    • MOA: provides hormones for corpus luteum , suppresses ovulation
  27. Progesterone - Effects
    Increase lipoprotein lipase, insulin, ketogenesis, body temp, aldosterone.

    Decreases Na resaborption, plasma AAs

    Adverse Effects: High BP, low HDL
  28. Progesterone Drug Names
    D - androgenic
    B- anabolic
    E- antiestrogen
    • Hydroxyprogesterone
    • Medroxyprogesterone - E, D (tx ovarian supression sx)
    • Megestrol - D
    • Dimethisterone
    • Desogestrol
    • Norethynodrel
    • Norethindrone - D, B, E (aldosterone SE)
    • Norgestel - D, B, E (aldosterone SE)
    • "No Retht during gestation- I will Di methis terone?"
  29. Clomiphene
    • SERM - selective estrogen receptor Modulators
    • 1. clomiphene
    • - clogs estrogen receptor at hypothalamus - increased GnRH
    • - Competitive antagonist
    • - Use: Breast Cancer
  30. Raloxifene
    • SERM - selective estrogen receptor Modulators
    • 2. Raloxifene
    • - partial agonist/antagonist
    • - agnosit for bone & adipocytes
    • - antagonist - breast & uterus
    • - Use: Breast Cancer
    • Roxy, Tamy, Tori are dirty whores that agonize and antagonize men.
  31. Tamoxifen, Toremifene
    • SERM - selective estrogen receptor Modulators
    • 3. partial agonist/ antagonist
    • - Use: Breast Cancer
    • - Chemoprevention for BRCA in women with increased risk of cancer.
    • - Two T-ifenes are trouble (due to increased risk of endometrial cancer)
    • - Roxy, Tamy, Tori are dirty whores that agonize and antagonize men.
  32. Danazol
    • Glucocorticoid antagonist (estrogen/progesterone antag)
    • inhibits steroidgenesis in ovary
    • USE: endometriosis
    • Side effects: hirtuism, deep voice, acne
    • Inhibits P450
    • Don't use with pregnant women

    Dan the Man, doesn't want to date pregnant women & stops steroidgenesis.
  33. Fulvestrant
    • Estrogen antagonist
    • MOA - binds to Estrogen Receptor and signals degradation
    • Use: Tamoxifen Resistant Breast cancer
    • "Not a women, he's a full transvestite that degrades anyone who tries to bind his hoo-ha (estrogen receptor)... also he goes where Tami don't dare!"
  34. Anastrozole & Letrozole
    • Aromatase Inhibitors
    • - non steroidal
    • Use: tamoxifen resistant Breast Cancer

    Ana & Letoya are skinny (don't do steroids) and go where Tami won't go
  35. Exemestane
    • Aromatase Inhibitor
    • - steroidal
    • - irreversible
    • - Use: Advanced Breast Cancer

    Executioner is buff on steroids, no going back, and last stand against breast cancer.
  36. Ketoconazole
    • Anti androgen
    • Inhibits cholesterol -> androgen synthesis
    • Inhibits P450
    • Use: treat prostate cancer
    • SE: reversible gynecomastia
  37. Finasteride
    • Anti Androgen
    • 5 alpha reductase inhibitor
    • decrease DHT
    • Use: alopecia, BPH
  38. Cyproterone
    • Androgen Receptor Antagonist
    • Use: hirsutism, prostate cancer
    • SE: liver tox, ED
  39. Androgen Receptor Antagonists - utamides
    • Flutamide
    • Bicalutamide
    • Nilutamide
    • Use: treat prostate cancer
    • SE: GI upset, gynecomastia, liver tox
  40. Androgen receptor antagonist- spirnolactone
    • Potassium sparing diuretic
    • Blocks androgen receptor
    • Use: hirstuism, Conn syndrome, HTN
    • SE: menstrual irregularity and gynecomastia
  41. GnRH analogs
    • Goserelin
    • Naferelin
    • Bruselin
    • Leuprolide
    • Decrease androgen (due to constant GnRH)
    • Use: prostate ca

    Bruce the goose is naftsy when he is leuse. He'll bite you right on your prostate!
  42. Androgen replacement tx: low anabolic activity
    • Testosterone (topical)
    • Testosterone propinate (IM)
    • Testosterone enanthate (IM)
    • Testosterone cypionate (IM)

    • Synthetic
    • Methyltestosterone (PO)
    • Fluoxymesterone (PO- 2x > androgenic activity)

    Test the meth infected with flu. - synthetics
  43. Androgen replacement tx: high anabolic activity
    • Oxymetholone
    • Oxandrolone (highest anabolic activity)
    • Nandrolone

    Andre is as big as an ox!
  44. Androgen replacement tx:
    Physiologic effects
    Use: hypogonadal men, protein anabolic agent (post sugery or burn pts), anabolic steroid abuse, ED

    Physiologic effects: secondary sex characteristics, decreases HDL, increases clotting factors and liver protein, increase renal erythropoietin, decrease excretion of nitrogen in urine

    SE: masculinizing in women and kids, acne, gynecomastia, Na retention to edema, hepatic dysfxn, BPH, CNS problems in infants
Card Set:
Hypothalamic and Pituitary Hormones
2012-03-12 00:27:49
hormone drugs

B3 drugs
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